Synthesis of 12-quinoline substituted andrographolide derivatives and their preliminary evaluation as anti-aggregation drugs

Based on the structure of natural product andrographolide, a series novel 12-quinoline substituted derivatives 9 were designed and synthesized. In preliminary biological evaluation, these synthesized compounds showed prominent anti-platelet aggregation activities in response to thrombin adenosine diphosphate (ADP) agonists. Among them, compound 9o (inhibition rate 55.73%, IC50 0.36 µM/L) had highest activity induced by ADP. Compound 9q 54.31%, 0.30 thrombin. Most no significant cytotoxicity. Our research results provide candidate drug for enrich scope application andrographolide derivatives.